Green synthesis of coumarin-pyrazolone hybrids: In vitro anticancer and anti-inflammatory activities and their computational study on COX-2 enzyme

A series of novel quinoline-2-carboxamides 4(a–l) were synthesized using different 2-oxo-2H-chromene-4-carbaldehyde and 3-methyl-1H-pyrazole-5(4H)-one with excellent yield under eco-friendly condition. All the compounds were confirmed on the basis of their IR, 1H NMR, 13C NMR and mass analysis. Newl...

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Bibliographic Details
Published in:Chemical Data Collections 2018-12, Vol.17-18, p.497-506
Main Authors: Kulkarni, Rashmi C., Madar, Jyoti M., Shastri, Samundeeswari L., Shaikh, Farzanabi, Naik, Nirmala S., Chougale, Ravindra B., Shastri, Lokesh A., Joshi, Shrinivas D., Dixit, Sheshagiri R., Sunagar, Vinay A.
Format: Article
Language:English
Subjects:
Anti-inflammatory activity
Anticancer activity
Computational study
Coumarin-pyrazolone
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Summary:A series of novel quinoline-2-carboxamides 4(a–l) were synthesized using different 2-oxo-2H-chromene-4-carbaldehyde and 3-methyl-1H-pyrazole-5(4H)-one with excellent yield under eco-friendly condition. All the compounds were confirmed on the basis of their IR, 1H NMR, 13C NMR and mass analysis. Newly synthesized compounds were screened for their anti-inflammatory by using protein denaturation method and anticancer activities at NCI60, Anti-inflammatory results are found to be promising. Further, molecular docking studies were performed for all the synthesized compounds with the active site of COX-2 enzyme and results obtained are quite promising. Compounds 4e and 4h exhibited highest potency and selectivity for COX-2 inhibitory activity. [Display omitted]
ISSN:2405-8300
2405-8300
DOI:10.1016/j.cdc.2018.11.004